Enzalutamide
| CAS No. | 915087-33-1 | Cat. No. | BCP02361 |
| Name | Enzalutamide | ||
| Synonyms | MDV-3100;MDV3100;MDV 3100; | ||
| Formula | C21H16F4N4O2S | M. Wt | 464.44 |
| Description | Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys).Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. | ||
| Pathways | Hormone Pathay | ||
| Targets | Androgen Receptor | ||
Structure
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